Epigenetics
Epigenetics research delves into the molecular mechanisms that control gene expression and cellular traits without altering the underlying DNA sequence. One crucial aspect of this field is the role of small molecules, which act as powerful regulators of epigenetic modifications. These small compounds, typically comprising a few dozen to a few hundred atoms, have emerged as essential tools in understanding and manipulating the epigenome.
- DNA Methylation Inhibitors: Small molecules like 5-azacytidine and 5-aza-2'-deoxycytidine are DNA methyltransferase inhibitors. They block the addition of methyl groups to DNA, leading to DNA demethylation. This can reactivate silenced genes, potentially offering therapeutic avenues for conditions like cancer.
- HDAC inhibitors: HDACs remove acetyl groups from histone proteins, contributing to gene repression. Small molecule HDAC inhibitors, such as Vorinostat and Romidepsin, can reverse this process by increasing histone acetylation, allowing genes to be more accessible for transcription. These inhibitors are being explored for cancer therapy and other conditions.
- Histone Methyltransferase Inhibitors: Small molecules like GSK126 inhibit specific histone methyltransferases, affecting histone methylation patterns. This can alter gene expression, making them promising candidates for cancer and other diseases with epigenetic dysregulation.
- RNA Modulators: Small molecules can also target non-coding RNAs involved in epigenetic regulation. For instance, small molecules called small interfering RNAs (siRNAs) can be designed to target and degrade specific long non-coding RNAs, influencing gene expression.
- Epigenetic Reader Domain Inhibitors: These small molecules target proteins that recognize and bind to specific epigenetic marks. Examples include inhibitors of bromodomain-containing proteins (BET inhibitors), which can disrupt gene regulation by interfering with protein-DNA interactions.
Small molecules in epigenetics research not only provide insights into the fundamental biology of gene regulation but also hold immense promise for developing novel therapeutics. Their ability to selectively modulate specific epigenetic marks and pathways has led to ongoing clinical trials and drug development efforts for various diseases, including cancer, neurological disorders, and inflammatory conditions. Understanding and harnessing the power of these small molecules is at the forefront of modern epigenetics research, offering new hope for precision medicine and targeted therapies.
3 key components involved in the regulation of epigenetic modifications
Epigenetics Writer
Epigenetics writers are enzymes responsible for adding chemical marks or modifications to DNA or histone proteins. These marks include DNA methylation (addition of methyl groups to DNA) and histone modifications (such as acetylation, methylation, phosphorylation, etc.).
Epigenetics Reader
Function: Epigenetics readers are proteins that can recognize and bind to specific epigenetic marks on DNA or histones. These reader proteins interpret the epigenetic code and facilitate downstream cellular processes, such as gene activation or repression.
Epigenetics Eraser
Function: Epigenetics erasers are enzymes responsible for removing or reversing epigenetic marks on DNA or histones. This process allows for the dynamic regulation of gene expression and the resetting of epigenetic states during various stages of development and in response to environmental changes.
Catalog No.
Product Name
Application
Product Information
Citations
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BRD4 PROTAC Ligand
(S)-JQ-35-Boc is a selective BRD4 PROTAC ligand that facilitates the synthesis of BRD4 targeted degraders, specifically RAJQ14. This compound plays a key role in research applications focused on cancer, providing a mechanism to explore the therapeutic potential of targeted protein degradation. Its use in the generation of RAJQ14 enables investigations into novel strategies for cancer treatment through the modulation of BRD4 activity. -
BRD9 degrader
PROTAC BRD9 Degrader-6 is a highly effective degrader targeting BRD9, exhibiting an IC50 of 0.13 nM. This compound selectively induces proteolysis of BRD9, facilitating the study of diseases associated with the BAF complex. It is a valuable tool for researchers investigating the role of BRD9 in various biological contexts and its potential therapeutic applications. -
BPTF Bromodomain Inhibitor
(S)-GSK1379725A is a selective inhibitor of the bromodomain and PHD finger containing transcription factor (BPTF) with a Kd of 2.8 μM. This compound demonstrates specificity for BPTF and does not significantly inhibit BRD4 bromodomain. Additionally, (S)-GSK1379725A exhibits antimalarial activity, making it a valuable tool for studying transcriptional regulation and potential therapeutic applications against malaria. -
EP300/CBP Inhibitor
EP300/CBP-IN-2 is a potent inhibitor of the EP300 and CBP histone acetyltransferases, targeting the regulation of gene expression involved in cancer biology. This compound demonstrates significant biological activity in vivo, making it a valuable tool for investigating the role of these targets in tumorigenesis and potential therapeutic interventions. Its applications extend to cancer research, exploring novel strategies for epigenetic modulation in cancer treatment. -
BET Inhibitor
BET-IN-9 is a Bromodomain and Extra-Terminal (BET) protein inhibitor that disrupts the interaction between BET proteins and acetylated lysines. This compound exhibits significant biological activity in blocking transcriptional regulation mediated by BET proteins. BET-IN-9 is utilized in research applications investigating cancer biology, inflammation, and other diseases associated with aberrant gene expression. -
BRD4-BD1 Inhibitor
BRD4-BD1-IN-1 is a selective inhibitor of the BRD4-BD1 interaction, exhibiting an IC50 value of 38.20 μM. This compound disrupts the binding of bromodomain-containing protein 4 to acetylated lysines, thereby modulating transcriptional regulation. It is valuable for research into the role of BRD4 in cancer and other diseases, making it a useful tool for understanding epigenetic mechanisms and developing novel therapeutic strategies. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-18 is a dual-target PROTAC degrader that selectively degrades the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It exhibits potent degradation activity with DC50 values of less than 100 nM in A549 cells for SMARCA2 and MV411 cells for SMARCA4. This reagent is useful for investigating the functional roles of SMARCA2 and SMARCA4 in cellular processes and may provide new insights into therapeutic strategies targeting chromatin remodeling in cancer research. -
BRD PROTAC Degrader
PROTAC BRD4 Degrader-26 is a photo-regulated PROTAC designed to selectively degrade BRD4 through a photocleavable linker. This compound achieves an impressive 80% degradation of BRD4 at a concentration of 1 μM, demonstrating significant potency. The degradation process can be controlled by UV light, allowing for precise temporal regulation of BRD4 levels. It is an essential tool for researchers investigating the role of BRD4 in various biological pathways and its potential as a therapeutic target. -
SMARCA2 Degrader
PROTAC SMARCA2/4-degrader-10 targets the selective degradation of SMARCA2, exhibiting a DC50 value of less than 100 nM. This compound serves as a valuable tool in cancer research, facilitating studies on tumor biology and the therapeutic potential of targeting the BRG1/BRM-associated factor complex. The design incorporates a ligand linked to a VHL ligand, enhancing the efficacy of the degrader in cellular environments. -
BRD4 Inhibitor
BRD4 Inhibitor-31 is a potent inhibitor of the bromodomain-containing protein 4 (BRD4), exhibiting inhibitory constants (Kis) of 0.234 μM and 0.295 μM for BRD4 bromodomains BD1 and BD2, respectively. This compound is utilized in research investigating the roles of BRD4 in inflammatory diseases, cancer progression, and AIDS pathogenesis. Its effectiveness in modulating BRD4 activity makes it a valuable tool for understanding the therapeutic potential in various disease contexts. -
PROTAC BRD3 Degrader
PROTAC BRD3 Degrader-1 is a potent and selective proteolysis-targeting chimera (PROTAC) designed to degrade BRD3. Its mechanism involves the targeted degradation of BRD3, leading to the downregulation of H3K18ac while sparing BRD2 and BRD4. This compound demonstrates significant efficacy in reducing intraocular inflammation in the experimental autoimmune uveitis mouse model and inhibits pro-inflammatory responses in microglial cells, making it a valuable tool for uveitis research. -
SMARCA2/4 Molecular Glue Degrader
SMARCA2/4 degrader-1 is a molecular glue degrader specifically targeting SMARCA2 and SMARCA4, exhibiting a DC50 value of 2.2 nM for SMARCA4. This compound functions by covalently bridging CUL4DCAF16 and CRL1FBXO22, leading to the efficient degradation of SMARCA2 and SMARCA4 proteins. It is utilized in research to understand the roles of these proteins in various biological processes and disease states, particularly in cancer biology and epigenetic regulation. -
Bromodomain Inhibitor
Bromodomain inhibitor-12 (edisylate) is a selective bromodomain inhibitor that targets bromodomain-containing proteins, which play critical roles in the regulation of gene expression. This compound exhibits significant biological activity in modulating transcriptional processes related to autoimmune and inflammatory diseases. Its application in research can enhance the understanding of pathogenic mechanisms and facilitate the development of novel therapeutic strategies. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-21 is a targeted protein degradation compound that selectively degrades the SMARCA2 protein through the ubiquitin-proteasome system. It demonstrates potent biological activity with a DC50 value of 10-50 nM in A549 cells and exhibits even greater efficacy in MV411 cells, achieving a DC50 of less than 1 nM for SMARCA2 while showing limited degradation of SMARCA4 (DC50 >100 nM). This compound is useful for investigating the functional roles of SMARCA2 in cancer biology and therapeutic development. -
CBP Inhibitor
CBP-IN-1 is a potent inhibitor of the CREB-binding protein (CBP) with an IC50 of 1.5 nM. Additionally, it inhibits CBP BRET and BRD4(1), demonstrating IC50 values of 690 nM and 3100 nM, respectively. CBP-IN-1 is valuable for research applications focused on transcriptional regulation and related signal transduction pathways. Its selective inhibitory profile makes it a useful tool in the study of diseases associated with CBP dysregulation. -
SMARCA2/4 Inhibitor
SMARCA2-IN-8 is a selective inhibitor of the SWI/SNF chromatin remodeling complexes SMARCA2 and SMARCA4, exhibiting potent activity with IC50 values of 5 nM and 6 nM, respectively. This compound effectively inhibits the proliferation of SMARCA2-mutated cancer cells, specifically SKMEL5, with an AAC50 of 5 nM and downregulates SMARCA2-dependent KRT80 gene expression at an AAC50 of 10 nM. SMARCA2-IN-8 demonstrates substantial antitumor efficacy and favorable pharmacokinetic properties in preclinical mouse models, making it a valuable tool for investigating chromatin remodeling in cancer research. -
BRD4 PROTAC Degrader
BRD4 degrader-6 is a dimeric PROTAC degrader targeting the BRD4 protein, demonstrating a DC50 of less than 0.1 μM. This compound facilitates the ubiquitination and subsequent degradation of BRD4, contributing to its anticancer properties. It serves as a valuable tool for studying BRD4-related pathways and potential therapeutic strategies in cancer research. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-6, a targeted degrader of SMARCA2 and SMARCA4, employs a proteolysis-targeting chimeric approach to facilitate the degradation of these proteins. This compound demonstrates significant potential in cancer research by selectively lowering SMARCA2/4 levels, thereby disrupting oncogenic signaling pathways. Its unique structure includes a ligand for SMARCA2/4 and a VHL ligand to promote ubiquitination and subsequent proteasomal degradation, making it a valuable tool for elucidating the role of these proteins in tumor biology. -
PROTAC BRD4/BRD2 Degrader
PROTAC BRD2/BRD4 degrader-1 is an effective PROTAC targeting the BET proteins BRD4 and BRD2 with high selectivity. This compound facilitates the rapid and reversible degradation of BRD4 and BRD2, while sparing BRD3, making it a powerful tool for research into solid tumors. Its composition includes a BET inhibitor, a linker, and thalidomide, which targets cereblon (CRBN) and cullin 4A. This degrader demonstrates potential in cancer therapeutics with a minimal cytotoxic effect on cells. -
p300/CBP Inhibitor
KB528 is a selective inhibitor of the histone acetyltransferases p300 and CBP, demonstrating low nM IC50 values against these targets while sparing other members of the KAT family. This compound modulates the IRF4 transcriptional network, leading to decreased expression of key oncogenes such as IRF4, MYC, CAV2, and IGLL5, as well as reduced levels of IKZF3 protein. KB528 has been shown to effectively induce apoptosis in multiple myeloma cells, making it a valuable tool for research in multiple myeloma and related oncological studies. -
BRD4 PROTAC Degrader
BRD-SF2 is a BRD4-targeted PROTAC degrader that facilitates the selective degradation of the BRD4 protein. With a DC50 of 17.2 μM, it utilizes a VHL ligand and a specific linker to induce proteasomal degradation. This compound is valuable for research applications in cancer biology and epigenetics, providing insights into the role of BRD4 in transcriptional regulation and cellular processes. -
Bivalent BET Inhibitor
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. It demonstrates strong binding affinity to BRD4 and BRDT family members, with Kd values ranging from 0.6 to 28 nM. GXH-II-052 exhibits significant antiproliferative activity and effectively reduces c-Myc expression. This compound is valuable for research in cancer biology and epigenetic modulation. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-7 is a selective inhibitor targeting the bromodomain of polybromo-1 (PBRM1). With an IC50 value of 0.29 μM, it demonstrates significant inhibitory activity for PBRM1-BD2. This compound is primarily utilized in cancer research, facilitating studies on the role of PBRM1 in tumorigenesis and therapeutic resistance. -
PI3Kδ/BET Inhibitor
PI3Kδ/BET-IN-1 is a selective inhibitor targeting both PI3Kδ and the bromodomain BRD4-BD1. With an IC50 of 112 nM for PI3Kδ and 19 nM for BRD4-BD1, this compound demonstrates potent antiproliferative effects in diffuse large B-cell lymphoma (DLBCL) cells. Its dual inhibition mechanism makes it a valuable tool for research into cancer biology and therapeutic development. -
Bet Inhibitor
SDR-04 is a highly selective BET inhibitor that targets the BRD4-BD1 domain. It demonstrates potent inhibition of cell proliferation in the MV4;11 cancer cell line, making it a valuable tool for investigating the role of BET proteins in oncogenesis. SDR-04 can be utilized in various research applications aimed at understanding cancer biology and developing novel therapeutic strategies. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4 degrader-36 is a selective dual degrader targeting SMARCA2 and SMARCA4, demonstrating DC50 values of 0.22 nM and 0.85 nM, respectively. This compound exhibits significant anti-cell proliferation activity, making it a valuable tool for research in cancer biology and epigenetic regulation. It employs a unique mechanism of action involving targeted protein degradation, which can provide insights into the functional roles of SMARCA2 and SMARCA4 in various cellular processes. -
Bivalent BET Inhibitor
NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor with high affinity for BRD4 and BRDT family proteins, exhibiting Kd values of 0.095 nM for BRD4-1, 0.32 nM for BRD4-2, and 5.5 nM for BRDT-2, among others. This compound demonstrates notable antiproliferative activity and effectively reduces c-Myc expression. NC-III-49-1 is valuable for research in cancer biology and therapeutic studies targeting BET-related pathways. -
BRDT-BD2 Inhibitor
CDD-1128 is a potent BRDT-BD2 inhibitor with an IC50 value of 521 nM. This compound is primarily utilized in studies focused on nonhormonal contraceptive agents, offering significant potential for advancing reproductive health research. Its selectivity toward the BRDT-BD2 domain makes it a valuable tool for elucidating the biological pathways involved in spermatogenesis. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-17 is an innovative PROTAC degrader designed to target the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF chromatin remodeling complex. This compound effectively induces the degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, exhibiting DC50 values of less than 100 nM for both targets. It presents a valuable tool for research studies focused on the modulation of chromatin dynamics and cancer biology. -
SMARCA2/SMARCA4 PROTAC degrader
PROTAC SMARCA2/4 degrader-39 is a selective degrader that targets the SMARCA2 (BRM) and SMARCA4 (BRG1) proteins through the PROTAC mechanism. This compound exhibits significant efficacy in promoting the degradation of these chromatin remodeling proteins, which is crucial in various oncological contexts, particularly non-small cell lung cancer and colorectal cancer. Researchers may find this degrader valuable for studying the molecular mechanisms underlying tumor growth and developing innovative therapeutic strategies. -
BRD4 Inhibitor
TAT-PiET is a cell-penetrating peptide that specifically inhibits the extra-terminal (ET) domain of bromodomain-containing protein 4 (BRD4). This reagent demonstrates significant biological activity by reducing levels of both BRD4 and JMJD6, thereby effectively inhibiting cell proliferation. TAT-PiET exhibits resilience against endocrine resistance in estrogen receptor alpha (ERα)-positive breast cancer cells, making it a valuable tool for cancer research, particularly within the context of breast cancer studies. -
BET Inhibitor
DDO-8926 is a potent and selective inhibitor of Bromodomain and Extra-Terminal (BET) proteins, targeting their role in the transcriptional regulation of pro-inflammatory cytokines. This compound has been shown to significantly alleviate mechanical hypersensitivity, making it an important tool for studying neuropathic pain. Its application in research can enhance the understanding of inflammation-related pain mechanisms and provide insights into potential therapeutic strategies. -
BRD4 Degrader
EN884 is a selective degrader of BRD4, functioning through a SKP1- and proteasome-dependent mechanism. This compound facilitates targeted protein degradation and is applicable in synthetic proteolysis targeting chimeras (PROTACs) research. EN884 is valuable for investigating the role of BRD4 in various biological processes and disease contexts. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-29 (Compound I-279) is a selective degrader aimed at the catalytic subunits of the SWI/SNF chromatin remodeling complexes, SMARCA2 and SMARCA4. This compound effectively induces the degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, achieving a degradation concentration (DC50) of less than 100 nM for both targets. It is designed for use in research focused on chromatin regulation, epigenetic modifications, and related therapeutic applications. -
BRD7/BRD9 Inhibitor
BRD7-IN-3 is a selective inhibitor targeting bromodomain-containing proteins BRD7 and BRD9, demonstrating IC50 values of 1.6 μM and 2.7 μM, respectively. This compound serves as a valuable tool in cancer research, particularly in studies focused on epigenetic regulation and transcriptional modulation. Its ability to disrupt the interaction between bromodomains and acetylated lysines makes it instrumental for investigations into the role of BRD7 and BRD9 in various disease pathways. -
BRD4 Ligand
PROTAC BRD4 ligand-4 serves as a ligand for the bromodomain-containing protein BRD4. It is utilized in the synthesis of PROTAC BRD4 Degrader-37, facilitating targeted protein degradation. This compound is valuable in research applications focused on modulating gene expression and studying the role of BRD4 in various biological processes, including cancer progression and inflammation. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-6 is a selective inhibitor of the PBRM1 bromodomain, exhibiting a potent IC50 value of 0.22 μM. This compound demonstrates significant antiproliferative activity and is valuable for investigating PBRM1-dependent cancer mechanisms. Its application in research may aid in the development of targeted therapies for cancers that rely on PBRM1 modulation. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-1 is a selective inhibitor targeting the bromodomain of PBRM1, exhibiting significant binding affinity with a Kd of 0.7 μM and an IC50 of 0.2 μM. This compound demonstrates potent inhibitory activity, making it a valuable tool for probing the role of PBRM1 in cancer biology. PBRM1-BD2-IN-1 is suitable for research applications focused on cancer mechanisms and the therapeutic potential of bromodomain inhibition. -
BRD9 Degrader
BRD9 Degrader-2 (Compound B11) is a potent BRD9 degrader, exhibiting a DC50 of less than 1.25 nM and a maximal degradation effect (Dmax) exceeding 75%. This compound effectively targets the BRD9 protein, facilitating its degradation and thus has widespread applications in cancer research. Researchers can utilize BRD9 Degrader-2 to explore the role of BRD9 in various cancer pathways and its potential as a therapeutic target. -
BRD4 PROTAC Degrader
RAJQ14 is a PROTAC degrader that selectively targets BRD4, facilitating its degradation through the ubiquitination-independent pathway. By binding to the 19S proteasome cap subunits RPN1, RPN10, RPN13, and USP14, RAJQ14 recruits BRD4 to the proteasome, promoting proteolytic degradation. This compound is an invaluable tool for cancer research, enabling studies of the mechanisms underlying BRD4 modulation and its role in tumor biology. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-28 is a selective PROTAC agent that targets SMARCA2, effectively inducing its degradation with a DC50 of 3 nM in HiBiT A549 cells. This compound utilizes a bifunctional mechanism, linking a ligand for SMARCA2 with an E3 ligase ligand, facilitating targeted protein degradation. It serves as a potent tool for research applications aimed at studying SMARCA2's role in cellular processes and its potential implications in cancer therapeutics. -
SMARCA2 Inhibitor
DCSM06 is a selective inhibitor of the bromodomain within the SWI/SNF chromatin remodeling complex SMARCA2, demonstrating an IC50 of 9.7 μM. This compound modulates chromatin accessibility and regulation of gene expression, making it a valuable tool for studying the role of SMARCA2 in various biological processes. Its application extends to cancer research and epigenetic regulation, providing insights into potential therapeutic strategies targeting chromatin remodeling pathways. -
BRDT-BD2/BRD4-BD2 Inhibitor
CDD-1349 is a selective inhibitor of the BRDT-BD2 and BRD4-BD2 bromodomains, demonstrating a sixfold selectivity for BRDT-BD2 over BRD4-BD2. With an IC50 value of 22 nM against BRDT, this compound serves as a valuable tool in the exploration of nonhormonal contraceptive agents. Its targeted activity makes it suitable for research focused on reproductive biology and potential contraceptive development. -
Prodrug Of KMT9 Inhibitor
KMT9-IN-1 is a prodrug of the KMT9 inhibitor that releases the active compound 7b upon hydrolysis by cellular esterases. This compound effectively targets KMT9, resulting in a reduction of H4K12me1 levels. KMT9-IN-1 exhibits notable antitumor activity against colon cancer and can be employed in research focused on prostate cancer and hepatocellular carcinoma. -
BET Inhibitor
BET-IN-13 is a potent inhibitor of Bromodomain and Extraterminal (BET) proteins, with an IC50 value of 1.6 nM. This compound effectively decreases the mRNA expression levels of pro-inflammatory cytokines, including TNF-α, IL-1β, IL-6, and NOS2, demonstrating significant anti-inflammatory activity. BET-IN-13 is valuable for research involving acute liver injury and other inflammatory conditions. -
BRD Inhibitor
CPI703 is a selective bromodomain (BRD) inhibitor that targets the BRD of the 5DBM complex. By binding to specific residues in the first domain, CPI703 disrupts protein-protein interactions, leading to the modulation of cellular processes linked to transcription regulation. This compound is utilized in various research applications, including studies on epigenetic regulation and the development of cancer therapeutics. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-19 is designed to target the catalytic subunits of the SWI/SNF complex, specifically SMARCA2 and SMARCA4. This potent degrader effectively leads to the degradation of SMARCA2 in MV411 and A549 cells with a DC50 of less than 100 nM, as well as SMARCA4 in MV411 with a similar DC50. It serves as a valuable tool for researching the functional roles of these proteins in cancer biology and therapeutic development. -
Molecular Glue BRD4 Degrader
BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue that selectively targets BRD4 for degradation by inducing a ternary complex with RNF126, an E3 ligase. This compound effectively promotes the degradation of both the long and short isoforms of BRD4 within cellular contexts. It serves as a valuable tool for investigating the roles of BRD4 in various biological processes and disease states, particularly in cancer research and therapeutic development. -
BET Inhibitor
RX-37 is a selective bromodomain and extraterminal (BET) inhibitor that targets BET bromodomain proteins, including BRD2, BRD3, and BRD4, with Ki values ranging from 3.2 to 24.7 nM. This compound demonstrates significant potential in cancer research by modulating gene expression pathways associated with oncogenesis. RX-37 is suitable for studies focused on the role of BET proteins in tumor biology and therapeutic interventions. -
BRD4 Inhibitor
BRD4 Inhibitor-40 primarily targets the bromodomain protein BRD4, inhibiting its binding domains BRD4-BD1 and BRD4-BD2 with IC50 values of 16.1 nM and 142.18 nM, respectively. This compound effectively modulates the expression of c-Myc and p21, resulting in G1 phase cell cycle arrest. Additionally, BRD4 Inhibitor-40 has demonstrated efficacy in inhibiting Pkd1-null renal cystic epithelial cells and blocking renal cyst formation in both Madin-Darby canine kidney and embryonic kidney vesicle models, thus showcasing its potential in renal research applications.
